The present invention relates to processes for the preparation of {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, a phosphoramidate derivative of aprepitant,
and pharmaceutically acceptable salts thereof, which is a useful therapeutic agent, specifically as a substance P (neurokinin-1) receptor antagonist.
This compound is disclosed as having therapeutic utility in U.S. Pat. Nos. 5,691,336 and 5,780,467 which also disclose processes of manufacture for this compound. In contrast to previously known processes, the present invention provides a more practical and economical method for preparing the compound in relatively high yield and purity. As such, there is a need for a process for the preparation of the compound that is cost-effective, amenable to large-scale production and utilizes readily available reagents.